SERT-IN-5
SERT-IN-5 is a potent, selective, and CNS-penetrant serotonin transporter (SERT) inhibitor with a Ki of 0.3 nM. SERT-IN-5 blocks serotonin reuptake to increase synaptic serotonin levels. SERT-IN-5 exhibits anti-anxiety effects in mice. SERT-IN-5 can be used for the research of anxiety, depression.
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- Fòrmula: C20H22N4O2
- Peso molecular:350.41
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Chemical Information
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Actividad biológica
Descripciòn
In Vitro
SERT-IN-5 (compound 21d) functionally inhibits serotonin reuptake in human SERT-transfected CHO cells with an IC50 of 4 nM[1].
SERT-IN-5 inhibits hERG ion channel function with an IC50 of 4 μM, showing low hERG potency[1].
SERT-IN-5 has excellent permeability in Caco-2 cells and MDR1-MDCKII cells[1].
SERT-IN-5 (10 μM) shows high selectivity across over 90 targets, with only 5-HT2B receptors having significant binding (Ki = 360 nM), representing 1000-fold selectivity over its SERT binding affinity, and no 5-HT2B agonist activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
SERT-IN-5 (3 mg/kg; i.p.; single dose) increases prefrontal cortex (PFC) levels of serotonin in SD rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Swiss mice (6 weeks)[1]
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Dosage:1 mg/kg
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Administration:s.c.; single dose; 30 min pre-testing
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Result:Modestly suppressed marble burying behavior alone.
Had substantially greater efficacy when combined with Pimavanserin (HY-14557).
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Animal Model:Male SpragueDawley rats (290-340 g)[1]
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Dosage:3 mg/kg
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Administration:i.p.; single dose
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Result:Alone induced a large increase in PFC levels of serotonin.
Induced substantially higher levels of all three neurotransmitters than either compound alone when combined with Pimavanserin.
Chemical Information
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Peso molecular 350.41
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Fòrmula C20H22N4O2
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SMILES
CNCC1=CC(C2=NC=C(C=N2)OC)=CC=C1OCC3=CN=C(C=C3)C
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SERT-IN-5 Related Classifications
HY-183269 Related Classifications
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